Raloxifene 60mg/ml , 60ML

Raloxifene 60mg/ml , 60ML

Brand: Full Catalog
Product Code: RX60
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Price: $60.00
Description

Raloxifene 60mg/ml, 60ML

Raloxifene (trade name Evista) is a selective estrogen receptor modulator (SERM) shown to increase testosterone in men, potentially treat adolescent gynecomastia, potentially kill prostate cancer cells, and help reverse bone density loss in osteoporosis including elderly male osteoporosis[1][2][3][4]. Like other SERMs, most similarly tamoxifen, raloxifene is used to treat ER-positive breast cancer[5]. Raloxifene may be a more benign alternative to tamoxifen in terms of ocular, carcinogenic, and other adverse side-effects[6][7][8].

Kastelan et al (2006) highlight the reasons raloxifene may be not only safer or with fewer adverse effects than tamoxifen but also a more suitable therapy for men:

SERMs may be useful for the prevention and treatment of osteoporosis not only in postmenopausal women but also in elderly men...Raloxifene has been shown to increase bone mineral density of the hip in men receiving androgen deprivation therapy for prostate cancer. Moreover, experimental data demonstrated dramatic increase in cell death in human prostate cancer cell lines after the treatment with raloxifene.[4]

The effects of raloxifene, similar to other SERMs, are primarily mediated through the estrogen receptor (ER), and although it is considered an anti-estrogen (estrogen receptor antagonist) in some tissues raloxifene acts as an ER agonist. It is from mimicking the effects of estrogen in various tissues that some of the atypical effects of raloxifene occur, such as increased bone mineral density.

Raloxifene has a positive effect as an adjunct treatment in schizophrenia, in men as well as women, possibly owing to the neurosteroid-like effect (similar to estrogen but without feminizing side-effects) of the compound functioning as an estrogen receptor agonist[9].

In animal models of Parkinson’s Disease, where estrogen has previously been shown to be neuroprotective, raloxifene was also found to be neuroprotective by Litim, Morissette, and Di Paolo[10].

Citations:

[1] Silverman SL. New selective estrogen receptor modulators (SERMs) in development. Curr Osteoporos Rep. 2010 Sep;8(3):151-3.

[2] Duschek EJ, Gooren LJ, Netelenbos C. Comparison of effects of the rise in serum testosterone by raloxifene and oral testosterone on serum insulin-like growth factor-1 and insulin-like growth factor binding protein-3.  Maturitas. 2005 Jul 16;51(3):286-93.

[3] Nordt CA, DiVasta AD.  Gynecomastia in adolescents. Curr Opin Pediatr. 2008 Aug;20(4):375-82.

[4] Kastelan D, Giljevic Z, Kraljevic I, Korsic M. Selective estrogen receptor modulators: A possible new treatment of osteoporosis in males. Med Hypotheses. 2006;67(5):1052-3.

[5] Christodoulakos G, Lambrinoudaki I, Panoulis C, Sioulas V, Rizos D, Caramalis G, Botsis D, Creatsas G. Serum androgen levels and insulin resistance in postmenopausal women: association with hormone therapy, tibolone and raloxifene.  Maturitas. 2005 Apr 11;50(4):321-30.

[6]Oncol Rep. 2004 Sep;12(3):517-21. Differential effects of raloxifene and tamoxifen on the expression of estrogen receptors and antigen Ki-67 in human endometrial adenocarcinoma cell line. Koda M1, Jarzabek K, Haczynski J, Knapp P, Sulkowski S, Wolczynski S.

[7]Grigsby JG, Parvathaneni K, Almanza MA, Botello AM, Mondragon AA, Allen DM, Tsin AT. Effects of tamoxifen versus raloxifene on retinal capillary endothelial cell proliferation.

J Ocul Pharmacol Ther. 2011 Jun;27(3):225-33.

[8]Siesky B, Harris A, Kheradiya N, Ehrlich R, Klaas C, Kaplan B, Catoira Y, McCranor L, Rospigliosi C, Harris M. The effects of raloxifene hydrochloride on ocular hemodynamics and visual function. Int Ophthalmol. 2009 Aug;29(4):225-30.

[9]Khodaie-Ardakani MR, Khosravi M, Zarinfard R, Nejati S, Mohsenian A, Tabrizi M, Akhondzadeh S. A Placebo-Controlled Study of Raloxifene Added to Risperidone in Men with Chronic Schizophrenia. Acta Med Iran. 2015;53(6):337-45.

[10]Litim N, Morissette M, Di Paolo T. Neuroactive gonadal drugs for neuroprotection in male and female models of Parkinson's disease.Neurosci Biobehav Rev. 2015 Dec 17. pii: S0149-7634(15)30067-1.

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